Drug intelligence / Profile preview

As4S4 + Fe3O4

Development stage
Preclinical
Lead developer
Institute of Geotechnics, Slovak Academy of Sciences
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
In Vitro, Ex Vivo, Intravenous
01

Overview

Composite nanoparticles of **arsenic sulfide (As4S4, also known as realgar) and magnetite (Fe3O4)** have been developed as multifunctional anticancer agents. These nanosuspensions are characterized by their ability to induce apoptosis and cell cycle arrest (G2/M), disrupt mitochondrial membrane potential, and downregulate oncogenic pathways such as c-Myc and p-PI3K. The mechanism of action primarily involves **caspase-dependent and mitochondria-dependent apoptosis**, with notable cell cycle effects (increase in cyclin B1, histones H2AX/H3, activation of ATR, Chk1/2) and suppression of stem cell-like populations. These nanoparticles activate cell signaling (p-ERK, p-JNK), show synergy with standard multiple myeloma therapies (e.g., dexamethasone, melphalan, bortezomib, lenalidomide, pomalidomide), and have demonstrated **anti-myeloma activity in vitro, ex vivo, and in vivo** models with limited toxicity toward normal cells. The composite offers both **therapeutic and magnetic functionalities** for potential in oncology, specifically multiple myeloma and possibly other cancers like breast and tongue carcinoma[1][2][3][4].

Other names
arsenic sulfide + magnetiterealgar + magnetite
02

Targets

JNK (Mitogen-activated protein kinase kinase kinase family)CCNB1 (Cyclin B1)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)MAPK3 (Mitogen-activated protein kinase 1)CHEK2 (Checkpoint kinase 2)Mitochondria-dependent apoptotic machineryMYC (MYC proto-oncogene protein)

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